当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Inhibitory effect of phenothiazine- and phenoxazine-derived chloroacetamides on Leishmania major growth and Trypanosoma brucei trypanothione reductase.

Inhibitory effect of phenothiazine- and phenoxazine-derived chloroacetamides on Leishmania major growth and Trypanosoma brucei trypanothione reductase.

Abstract：

:A number of phenothiazine-, phenoxazine- and related tricyclics-derived chloroacetamides were synthesized and evaluated in vitro for antiprotozoal activities against Leishmania major (L. major) promastigotes. Several analogs were remarkably potent inhibitors, with antileishmanial activities being comparable or superior to those of the reference antiprotozoal drugs. Furthermore, we explored the structure-activity relationships of N-10 haloacetamides that influence the potency of such analogs toward inhibition of L. major promastigote growth in vitro. With respect to the mechanism of action, selected compounds were evaluated for time-dependent inactivation of Trypanosoma brucei trypanothione reductase. Our results are indicative of a covalent interaction which could account for potent antiprotozoal activities.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Marcu A,Schurigt U,Müller K,Moll H,Krauth-Siegel RL,Prinz H

doi

10.1016/j.ejmech.2015.11.023

subject

Has Abstract

pub_date

2016-01-27 00:00:00

pages

436-443

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30359-7

journal_volume

108

pub_type

杂志文章

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